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Differences between various heparin

2022-05-23
Differences between various heparin

Since heparin was discovered, it is still widely used in the prevention and treatment of various thromboembolic diseases due to its rapid onset of action, definite curative effect and reversible anticoagulant effect. However, there are many types of heparin with similar names, such as blood collection tube additive heparin, low molecular weight heparin, enoxaparin, nadroparin, etc., which can easily lead to mutual confusion. What are the types of heparin and what are the differences between each type of heparin? Today Desheng takes you to find out.

Heparin is mainly divided into unfractionated heparin (UFH), blood collection tube additive heparin, low molecular weight heparin (LMWH), heparin derivatives (such as fondaparinux sodium), and heparin analogs (such as danaparin).

 

Types of heparin

Unfractionated heparin is a mixture of sulfated glycosaminoglycans (GAGs). It is a mucopolysaccharide sulfate alternately composed of D-glucosamine, L-iduronic acid and D-glucuronic acid, which can be prepared from the lungs of cattle or the intestinal mucosa of cattle, sheep and pigs.

Vacuum blood collection tube anticoagulant heparin (sodium heparin or lithium heparin) is an additive in blood collection tubes. It is used in anticoagulant tubes to prevent blood coagulation in vitro after blood collection for a certain period of time. This heparin is usually not of injection grade. It is different from heparin drugs, but its potency is relatively high.

Heparin for Cosmetic raw material can be added to nutritional creams, eye creams, acne-removing products and hair growth agents, etc. It has many functions like increasing the vascular permeability of the skin,improving local vascular circulation,promoting the supply of skin nutrients and the excretion of metabolic wastes. It Plays a good role in health care and maintenance of the skin.

Heparin with low molecular weight is a short-chain preparation obtained from the separation or degradation of unfractionated heparin. Due to differences in molecular size, anticoagulant activity, preparation method, and manufacturer, commonly used clinical heparins with low molecular weight include enoxaparin, dalteparin, and nadroparin.

 

Differences between various heparin

Different molecular weight

The molecular weight range of unfractionated heparin is 3000~30000Da, and the average molecular weight is 15000Da, which is equivalent to 45 sugar units. The molecular weight of low molecular weight heparin is about 1/3 of that of unfractionated heparin, and the molecular weight of fondaparinux is the smallest, only 1728Da. The size of the molecular weight is closely related to the anticoagulant activity and mechanism of action of the drug.

 

Different mechanism of function

The anticoagulant effect of heparin is mainly mediated by antithrombin III (AT-III). Heparin molecule combines with AT-III lysine residue to form a reversible complex, which changes the AT-III configuration.Then the active site of arginine fully exposed to rapidly bind with the serine active center of IIa (thrombin),IXa, Xa, XIa,etc. It accelerates the inactivation of coagulation factors.

When heparin inactivates factor IXa/IIa by AT-III, it must combine with AT-III and coagulation factor to form a ternary complex, while when inactivating by factor Xa, it only needs to combine with AT-III. Once the heparin-AT-III-coagulation factor complex is formed, heparin is dissociated from the complex, combined with another molecule of AT-III for repeated use.

 

Different pharmacokinetic properties

Unfractionated heparin can be injected subcutaneously, intravenously or intravenously, but its bioavailability is low during subcutaneous injection, and its elimination in vivo is dose-dependent. In addition, the plasma protein binding rate of unfractionated heparin is as high as 80%, and most of them also bound to endothelial cells, macrophages, etc. That makes its anticoagulant activity unpredictable. Compared with unfractionated heparin, low molecular weight heparin has obvious pharmacokinetic advantages. After subcutaneous injection, the bioavailability of low molecular weight heparin can reach 90%, and the plasma protein binding rate is low, so the anticoagulant effect is more predictable than unfractionated heparin.

 

It should be noted that the heparin currently produced and developed by Desheng (sodium heparin and lithium heparin) is mainly used as anticoagulant in blood collection tubes.It can neither be injected nor used as a medicinal grade. Its potency is relatively high, generally between 150IU-180IU. Of course, a higher potency can be customized. But the higher the potency, the more expensive the price. If you have purchasing requirements, please contact for details!